NPS-2143

- Overview
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    Background
    
    NPS-2143 is a novel and selective antagonist of CaSR (Ca2+-sensing receptor) with the EC50 value of 4.27mM for [Ca2+]o [1].Calcilytics NPS-2143 has been reported to diminish the sensitivity of the CaSR for [Ca2+]o, resulting in an attenuated signal transduction in vitro and increased secretion of PTH in vivo. In addition, The EC50 values of NPS-2143 are 4.27, 1.56, 1.61, 2.46, 2.07 and 3.15mM for the wild-type CaSR, mutant CaSR (T151R, P221L, E767Q, G830S, and A844T), respectively. Apart from these, in HEK 293T cells expressing CaSR, NPS-2143 has been revealed to inhibit the [Ca2+]o-induced cytosolic calcium signal in a concentration-dependent manner [1].
    
    [1] Letz S1, Rus R, Haag C, Dörr HG, Schnabel D, Möhlig M, Schulze E, Frank-Raue K, Raue F, Mayr B, Schöfl C. Novel activating mutations of the calcium-sensing receptor: the calcilytic NPS-2143 mitigates excessive signal transduction of mutant receptors. J Clin Endocrinol Metab. 2010 Oct;95(10):E229-33. .
- Properties
  - Categories
    
    CaSR antagonist
    
    Alternative Name
    
    2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile
    
    CAS Number
    
    284035-33-2
    
    Molecular Formula
    
    C24H25ClN2O2
    
    Molecular Weight
    
    408.93
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥40.9 mg/mL in DMSO; insoluble in H2O; ≥28.35 mg/mL in EtOH
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    CC(C)(CC1=CC2=CC=CC=C2C=C1)NCC(COC3=C(C(=CC=C3)Cl)C#N)O
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

NPS-2143

Background

Documents

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